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Assay Detail

CHEMBL649916

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Type-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
Chakravarty PK, Naylor EM, Chen A, Chang RS, Chen TB, Faust KA, Lotti VJ, Kivlighn SD, Gable RA, Zingaro GJ.
J Med Chem (1994) 37 : 4068 -4072
PubMed 7990105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.04 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335778 1 5.75
CHEMBL336180 1 5.62
CHEMBL293511 1 5.54
CHEMBL131156 1 5.44
CHEMBL191 LOSARTAN 4.0 1 4.30
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 4.30
CHEMBL7550 L-158809 1 4.30
CHEMBL334670 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335778 IC50 = 1800.0 nM 5.75
CHEMBL336180 IC50 = 2400.0 nM 5.62
CHEMBL293511 IC50 = 2900.0 nM 5.54
CHEMBL131156 IC50 = 3600.0 nM 5.44
CHEMBL191 LOSARTAN IC50 = 50000.0 nM 4.30
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 50000.0 nM 4.30
CHEMBL7550 L-158809 IC50 = 50000.0 nM 4.30
CHEMBL334670 IC50 > 10000.0 nM -